Test #5 Pain Flashcards
What is the prototype drug for steroidal anti-inflammatory drugs
Corticosterone
Where does the corticosteroid work in order to block the pain preception?
It inhibits the PLA2 which stops the entire cascade which inhibits prostaglandin and leukotriene synthesis
What are some SE from the treatment with steroids?
immunosuppression, adrenal insufficiency upon withdrawal, and fever
What is one major SE when on steroids because we are inhibiting the prostaglandin production?
Stomach ulcers because we are inhibiting prostaglandins which usually protect the lining of the stomach.
Where exactly do non-steroid anti-inflammatory drugs work?
They work by inhibiting COX1 and COX2 which block nociepotor sensitization and they also reduce leukocyte invasion
what is the prototype drug for non-steroid anti-inflammatory drugs?
ibuprofen
What is a SE from non-steroid anti-inflammatory drugs? They are weak acids so must take with food or water to prevent ulcers
GI upset - bc COX1 normally protects the lining of the stomach
WhAT non-steroid anti-inflammatory drug HAS A REVERSIBLE inhibition of platelet aggregation and in an injectable form that resembles morphine
Ketorolac
What are three COX2 inhibitors that have less GI SE because they don’t inhibit COX1?
Celeboxib - Celebrex
Robecoxib - Vioxx
Valdecoxib
What are three non-steroid anti-inflammatory drugs that are used to treat Rheumatoid Arthritis (chronic inflam. pain?
Diclofenac
Indomethacin
Piroxicam
What are three non-steroid anti-inflammatory drugs used to treat Osteoarthrosis? (phasic inflm pain)
Diclofenac
ibuprofen
ketoprofen
What are 4 non-steroid anti-inflammatory drugs to treat Post-op pain or acute pain
Diclofenac
ibuprofen
ketoprofen
Flurbiprofen
What are three non-steroid anti-inflammatory drugs to treat HE
Naproxen
ibuprofen
ketoprofen
What is one drug that is NOT an NSAID but is used for pain
Acetaminophen
What is the main action of acetaminophen?
On the CNS - NOT the site of the pain
you need a very high dose (lethal) for inhibit COX
Where is acetaminophen metabolized? and where is it excreted?
metabolized in the liver (p450) and excreted by the kidneys - retarded in the elderly and liver disease patients
What drug is used for an OD of acetaminophen? you must take within 4 hours to protect liver/prevent damage.
N-acetylcysteine
This increases glutathione production - a protective hormone in the liver
What are three indications for the use of acetaminophen?
HE - some forms (not migraines)
Fever - in kids esp)
Osteroarthritis - its a mechanical disease - not inflammatory
What is the prototype drug for opioids? and what receptor does it work on and what is that receptors NT?
Morphine —>mu receptors —–> endorphins
Name each of the primary NT for each of the receptors.
Mu
Kappa
Delta
mu - endorphins
Kappa - dynorphins
Delta - enkephalins
What is the #1 universal effect of morphine? everyone gets it? you NEVER develop a tolerance to
and what is another one you never develop a tolerance to?
2 - you don’t develop a tolerance to constipation
Constipation!!
Mitosis - pin-point pupils
What are three WD symptoms of morphine?
hyperalgesia, goose flesh, and Dilated pupils
What is responsible for the metabolism of morphine? the active form—and is 100x more potent and responsible for most of the effects?
Morphine -3B-glucuronide
What drug is about 1/10th the potency of morphine and 5-7% of pt don’t possess the enzyme for the drug to work (CYP450 2D6)
Codeine
Codeine is a pro-drug so what enzyme do you need in-order to convert this drug into morphine so it can work?
CYP450 - 2D6
What drug is the same as morphine so its 10x more potent than Codeine? it is also metabolized by the same enzyme (CYP450 - 2D6)
Oxycodone
controlled release formula - OxyContin)
What drug is just like oxycodone but is given with acetaminophen to get better analgesia at a lower dose?
Hydrocodone
What drug crosses the BBB, 2-4x more potent than morphine, but has the same efficacy and SE just quicker
Heroin - mu receptor
What drug is 8-10x more potent than morphine. 4hrs duration and is available as a suppository
Hydromorphone (Dilaudid)
also Oxymorphone (Numorphan)
What drug is synthetic form of morphine that’s 4hr duration, decreases sm muscle spasms (good for post surgery) no mitosis.
Meperidine
Normaperidine is a toxic metabolite that can build up and cause seizures
What drug is synthetic form of morphine that is 100x potent, fast onset, short duration < 5 min so must be on continuous infusion. or a lolly pop
Fentanyl
What drug is synthetic form of morphine but is 4x more potent orally. 24hr t1/2,
Used to tx narcotic dependence
Methadone
What is the main opioid antagonist? it has a 99% first pass effect so give it IV and short t1/2 so give it often
Naloxone - Narcan
What drug is an antagonist at Mu and an agonist at Kappa and Delta. Naloxone was added so it has no effect and was kept on the market
Pentazocine - Talwin NX
What drug is an antagonist at Mu and an agonist at Kappa. Is a nasal spray and is 5x more potent in women than men bc of the hormone receptor is bind to
Butorphonal - Stadol
What drug is an antagonist at Mu and an agonist at Kappa. Dysphoria at high doses, common in ambulances so they won’t steal the morphine
Nalbuphine
What drug is a partial agonist at Mu and at Kappa3
Antagonist at Kappa1. Used by ex-drug abusers
Buprenorphine
What drug is an agonist at Mu and Delta.
A NE and 5-HT reuptake blocker (antidepressant)
Which these two action are synergistic for analgesia - they feel good!!!
Tramadol
